PRMT5-IN-34--生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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PRMT5-IN-34

Cat.No.:HY-158143

分⼦式:C₂₃H₁₉F₂N₅O₂

分⼦量:435.43

作⽤靶点:HistoneMethyltransferase

作⽤通路:Epigenetics

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PRMT5-IN-34(CompoundC)是MTA-cooperative蛋⽩质精氨酸甲基转移酶5(PRMT5/MAT)的抑制剂[1]。

IC50TargetPRMT5

体外研究PRMT5-IN-34inhibitseachcellproliferationactivitywithIC50=0.827μM(HDLM2),0.252μM(L540),0.077μ

M(L1236),4.638μM(L428),0.170μM(HCT116),8.538μM(HCT116)and0.538μM(HCT116),respectively

[1].

体内研究PRMT5-IN-34(p.o.;25-100mg/kg;oncedailyfor21days)inhibitstumorgrowthanddecreasesSDMA

proteinlevelsintheMTAP-silencedL540HLxenograftmousemodel[1].

AnimalModel:MTAPsilencedL540HLxenograftmodel[1]

Dosage:25;50;100mg/kg

Administration:p.o.oncedailyfor21days

Result:Concentration-dependentlyinhibitedtumorgrowth(22%,52%,93%).Concentration-

dependentlydecreasedtheproteinlevelofSDMA(83.9%,97.6%,99.1%).

REFERENCES

[1].JamesTetal.Methylthi